Priprava i evaluacija hidrogela s diazepamom za rektalnu primjenu

Diazepam (DZP) has become a commonly used drug for treatment of acute repetitive epileptic seizures and febrile convulsions in children. Considering the advantages of rectal administration of DZP, the objective of our study was to formulate and evaluate rectal hydrogels containing DZP as a drug substance in combination with suitable co-solvents and preservatives. Prepared HPMC (hydroxypropyl methylcellulose) hydrogels containing different concentrations of DZP (2, 4 and 6 mg mL-1) manifested good quality in respect to physico-chemical parameters (pH value, drug content, ingredients content and viscosity), antimicrobial efficiency and microbiological quality. Under the proposed HPLC conditions, satisfactory separation of DZP and the preservatives used was achieved. In vitro release studies have shown that the total amount of DZP was released in a period of 3 h. Prepared formulations were stable for four months at 26 oC (ambient temperature characteristic of the 2nd climate zone).Diazepam (DZP) je ljekovita tvar koja se upotrebljava u terapiji akutnih epileptičkih napada i febrilnih konvulzija u djece. U radu je opisana priprava i evaluacija hidrogela za rektalnu primjenu s diazepamom i odgovarajućim pomoćnim tvarima i konzervansima. Pripravci su sadržavali različite koncentracije DZP (2, 4 i 6 mg mL-1). Njihova fizičko-kemijska svojstva (pH vrijednost, sadržaj ljekovite i pomoćnih tvari, viskoznost), antimikrobna učinkovitost i mikrobiološka čistoća bili su zadovoljavajući. Razvijena je HPLC metoda kojom je postignuta separcija DZP i konzervansa. In vitro ispitivanja su pokazala da se cjelokupna količina DZP oslobodi tijekom 3 h. Pripravci su bili stabilni 4 mjeseca na temperaturi 26 C (sobna temperatura karakteristična za 2. klimatsku zonu)

Priprava i evaluacija hidrogela s diazepamom za rektalnu primjenu

Diazepam (DZP) has become a commonly used drug for treatment of acute repetitive epileptic seizures and febrile convulsions in children. Considering the advantages of rectal administration of DZP, the objective of our study was to formulate and evaluate rectal hydrogels containing DZP as a drug substance in combination with suitable co-solvents and preservatives. Prepared HPMC (hydroxypropyl methylcellulose) hydrogels containing different concentrations of DZP (2, 4 and 6 mg mL-1) manifested good quality in respect to physico-chemical parameters (pH value, drug content, ingredients content and viscosity), antimicrobial efficiency and microbiological quality. Under the proposed HPLC conditions, satisfactory separation of DZP and the preservatives used was achieved. In vitro release studies have shown that the total amount of DZP was released in a period of 3 h. Prepared formulations were stable for four months at 26 oC (ambient temperature characteristic of the 2nd climate zone).Diazepam (DZP) je ljekovita tvar koja se upotrebljava u terapiji akutnih epileptičkih napada i febrilnih konvulzija u djece. U radu je opisana priprava i evaluacija hidrogela za rektalnu primjenu s diazepamom i odgovarajućim pomoćnim tvarima i konzervansima. Pripravci su sadržavali različite koncentracije DZP (2, 4 i 6 mg mL-1). Njihova fizičko-kemijska svojstva (pH vrijednost, sadržaj ljekovite i pomoćnih tvari, viskoznost), antimikrobna učinkovitost i mikrobiološka čistoća bili su zadovoljavajući. Razvijena je HPLC metoda kojom je postignuta separcija DZP i konzervansa. In vitro ispitivanja su pokazala da se cjelokupna količina DZP oslobodi tijekom 3 h. Pripravci su bili stabilni 4 mjeseca na temperaturi 26 C (sobna temperatura karakteristična za 2. klimatsku zonu)

Circulating sST2 and catestatin levels in patients with acute worsening of heart failure: a report from the CATSTAT‐HF study

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Mass and ionic composition of atmospheric fine particles over Belgium and their relation with gaseous air pollutants

Original article can be found at: http://www.rsc.org/publishing/journals/EM/Index.asp Copyright Royal Society of Chemistry. DOI: 10.1039/b805157gMass, major ionic components (MICs) of PM2.5, and related gaseous pollutants (SO2, NOx, NH3, HNO2, and HNO3) were monitored over six locations of different anthropogenic influence (industrial, urban, suburban, and rural) in Belgium. SO42-, NO3- NH4+, and Na+ were the primary ions of PM2.5 with averages diurnal concentrations ranging from 0.4-4.5, 0.3-7.6, 0.9-4.9, and 0.4-1.2 g/m3, respectively. MICs formed 39% of PM2.5 on an average, but it could reach up to 80-98 %. The SO2, NO, NO2, HNO2, and HNO3 levels showed high seasonal and site-specific fluctuations. The NH3 levels were similar over all the sites (2-6 g/m3), indicating its relation to the evenly distributed animal husbandry activities. The sulfur and nitrogen oxidation ratios for PM2.5 point towards a low-to-moderate formation of secondary sulfate and nitrate aerosols over five cities/towns, but their fairly intensive formation at the rural Wingene. Cluster analysis revealed the association of three groups of compounds in PM2.5; (i) NH4NO3, KNO3; (ii) Na2SO4; and (iii) MgCl2, CaCl2, MgF2, CaF2, corresponding to anthropogenic, sea-salt, and mixed (sea-salt + anthropogenic) aerosols, respectively. The neutralization and cation-to-anion ratios indicate that MICs of PM2.5 appeared mostly as (NH4)2SO4 and NH4NO3 salts. Sea-salt input was maximal during winter reaching up to 12 % of PM2.5. The overall average Cl-loss for sea-salt particles of PM2.5 at the six sites varied between 69 and 96 % with an average of 87 %. Principal component analysis revealed vehicular emission, coal/wood burning and animal farming as the dominating sources for the ionic components of PM2.5.Peer reviewe

Evaluation of the in vitro bee venom release and skin absorption from bioadhesive gel formulation

Topical and transdermal drug delivery are one of the most suitable alternative, non-invasive routes for administration of drugs in clinical practice mainly due to the increased patient compliance and reduced systemic drug side effects. Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected, as for example, topical formulations for the treatment of different local skin disorders. Also, significant concentrations of drug could be absorbed by the body regions close to the site of delivery, where regional effects are expected, for e.g., in the muscles, local blood vessels and articulations. Arthritis is a systemic, autoimmune disease characterized by inflammation of joints. Inflammatory cytokines cause activation of the macrophages which leads to swelling of joints, damage to cartilage, bone erosion , functional impairment and stiffness. Bee venom (BV) contains a variety of peptides, including melittin, apamin, adolapin, the mast-cell degranulating peptide, enzymes (phospholipase [PL] A2), biologically active amines (histamine and epinephrine) and nonpeptide components with anti�inflammatory, anti-arthritis, anticoagulant, antimicrobial, anticancer and anti-nociceptive properties. Melittin, a major peptide component of BV shown to have anti-inflammatory and anti�arthritis properties and inhibitory activity on nuclear factor kappaB which is involved in the synthesis of inflammatory mediators and may be essential for the treatment of arthritis using BV. The aim of this study was to evaluate the stability of crude BV as an active ingredient, as well as to evaluate the in vitro release and skin absorption of BV from a designed topical gel formulation

“Emotional Exhaustion and Perceived Corporate Social Responsibility: A Case Study of a Port Logistics Organization”

In an era of economic crisis, and at the shadow of major ethical scandals in organizations, Corporate Social Responsibility (CSR) strategy has emerged as a crucial element to reestablish the bond between corporations and all other stakeholders such as the local community, society and labor force. Crisis makes employees more stressful, since they work on unwarranted jobs causing them emotional exhaustion. This study aims to examine the association between employee emotional exhaustion and perceived corporate social responsibility (CSR). For this purpose, this study conducted a survey which examines if CSR (ethical, social, environmental dimensions) is negatively related to emotional exhaustion of employees on a sample of 93 employees of a port logistics management services organization. A structured questionnaire was developed in order to measure emotional exhaustion and employee perceptions about CSR activities. Building on the claim that employee perceptions of CSR activities may significantly related to emotional state, this paper examines three CSR dimensions (social, ethical and environmental) and emotional exhaustion. The results of this study indicate that environmental CSR exerts a negative significant effect on Emotional exhaustion. These finding will be of great value as they can contribute on understanding the impact of environmental CSR on emotional exhaustion with detrimental effects on employees’ productivity, job performance, and creativity. The importance of CSR environmental aspects and the relative strategies guiding CSR impact on emotional exhaustion affecting job-related outcomes are also discussed

Epitaxial growth of Bi₁₂GeO₂₀ thin film optical waveguides using excimer laser ablation

Thin-film optical waveguides of the photorefractive optical material bismuth germanium oxide (Bi12GeO20) have been epitaxially grown onto heated zirconia substrates by excimer laser ablative sputtering. The epitaxial nature and stoichiometry of the films were verified using x-ray diffraction analysis. Waveguide modes were observed for effective refractive indices in close agreement with theoretical predictions

Type 2 Diabetes Mellitus and Sarcopenia as Comorbid Chronic Diseases in Older Adults: Established and Emerging Treatments and Therapies

Type 2 diabetes mellitus (T2DM) and sarcopenia (low skeletal muscle mass and function) share a bidirectional relationship. The prevalence of these diseases increases with age and they share common risk factors. Skeletal muscle fat infiltration, commonly referred to as myosteatosis, may be a major contributor to both T2DM and sarcopenia in older adults via independent effects on insulin resistance and muscle health. Many strategies to manage T2DM result in energy restriction and subsequent weight loss, and this can lead to significant declines in muscle mass in the absence of resistance exercise, which is also a first-line treatment for sarcopenia. In this review, we highlight recent evidence on established treatments and emerging therapies targeting weight loss and muscle mass and function improvements in older adults with, or at risk of, T2DM and/or sarcopenia. This includes dietary, physical activity and exercise interventions, new generation incretin-based agonists and myostatin-based antagonists, and endoscopic bariatric therapies. We also highlight how digital health technologies and health literacy interventions can increase uptake of, and adherence to, established and emerging treatments and therapies in older adults with T2DM and/or sarcopenia

Towards sustainable polymeric nano-carriers and surfactants: facile low temperature enzymatic synthesis of bio-based amphiphilic copolymers in scCO2

We demonstrate that useful bio-based amphiphilic polymers can be produced enzymatically at a mild temperature, in a solvent-free system and using renewably sourced monomers, by exploiting the unique properties of supercritical CO2 (scCO2). We present the use of a novel near-ambient temperature approach to prepare renewable amphiphilic ABA copolymers in scCO2. Bio-based commercially available monomers have been polymerised to prepare chains with targeted molecular weight. The amphiphilic materials were prepared by end-capping the synthesised polymers with methoxy poly(ethylene glycol) (MPEG) chains in a one-pot high pressure reaction utilising Candida Antarctica Lipase B (CaLB) as a catalyst at a temperature as low as 35 °C. The block copolymers are characterised by 1H-NMR, GPC and DSC in order to carefully assess their structural and thermal properties. These polymers form self-assembled aggregates in aqueous environment and these nanostructures are studied through DLS, TEM and UV-Vis. Highly hydrophobic Coumarin-6 was used as a model to prove dispersion in water of lipophilic molecules. Maximum bubble pressure tests demonstrate the reduction in surface tension of these polymers and comparisons are made directly to commercial polymeric non-ionic surfactants

PDE8 Regulates Rapid Teff Cell Adhesion and Proliferation Independent of ICER

BACKGROUND: Abolishing the inhibitory signal of intracellular cAMP by phosphodiesterases (PDEs) is a prerequisite for effector T (Teff) cell function. While PDE4 plays a prominent role, its control of cAMP levels in Teff cells is not exclusive. T cell activation has been shown to induce PDE8, a PDE isoform with 40- to 100-fold greater affinity for cAMP than PDE4. Thus, we postulated that PDE8 is an important regulator of Teff cell functions. METHODOLOGY/PRINCIPAL FINDINGS: We found that Teff cells express PDE8 in vivo. Inhibition of PDE8 by the PDE inhibitor dipyridamole (DP) activates cAMP signaling and suppresses two major integrins involved in Teff cell adhesion. Accordingly, DP as well as the novel PDE8-selective inhibitor PF-4957325-00 suppress firm attachment of Teff cells to endothelial cells. Analysis of downstream signaling shows that DP suppresses proliferation and cytokine expression of Teff cells from Crem-/- mice lacking the inducible cAMP early repressor (ICER). Importantly, endothelial cells also express PDE8. DP treatment decreases vascular adhesion molecule and chemokine expression, while upregulating the tight junction molecule claudin-5. In vivo, DP reduces CXCL12 gene expression as determined by in situ probing of the mouse microvasculature by cell-selective laser-capture microdissection. CONCLUSION/SIGNIFICANCE: Collectively, our data identify PDE8 as a novel target for suppression of Teff cell functions, including adhesion to endothelial cells